Novel Anti-inflammatory Inhibitors of Phospholipase A2

UC San Diego researchers have developed a novel class of potent inhibitors of phospholipase A2 (PLA2), an enzyme that initiates the inflammatory cascade by releasing arachidonic acid and other inflammatory mediators. Current anti-inflammatories such as Celebrex and Vioxx target the cyclooxygenase enzymes (COX) that are just downstream from PLA2. Inhibition of PLA2 blocks the protaglandin cascade, as well as the leukotriene and platelet activating factor cascades. Since PLA2 supplies the substrate arachidonic acid, inhibition of PLA2 will also regulate the COX enzymes. The effectiveness of the PLA2 inhibitor has been demonstrated in vitro, and it is being tested in animal models of pain and inflammation.

File Number: 19183 

Web site: http://techtransfer.universityofcalifornia.edu/...

Disease: Central Nervous System